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Abstract: The aim of this study was to test the effects of age and chronic exercise training on antioxidant and heat shock protein (Hsp) expression by comparing the hearts of young (Y), sedentary old (SO) and trained old (TO) rats. In SO rats, there were: (a) changes in myocardial structure and function; (b) increased malondialdehyde levels; (c) no changes in superoxide-dismutase (SOD) enzymes; (d) reduced Hsp70 expression; and (e) increased Hsp27 expression. In TO rats, SOD enzymes and Hsp70 expression were increased and Hsp27 was further increased. Malondialdehyde level did not differ between TO and SO rats, which shows that chronic exercise did not affect the peroxidation index. In summary, by increasing Hsp27 and Hs70 levels, prolonged exercise partially counterbalanced the heart age-related effects in the antioxidant system without altering peroxidation levels. These findings suggest that the beneficial effects on aged-related cardiovascular changes could be connected to the “anti-oxidant” effects of prolonged exercise training. [Copyright &y& Elsevier]

Abstract: Two series of N-[5-oxo-4-(arylsulfonyl)-4,5-dihydro-1,3,4-thiadiazol-2-yl]-amides were synthesized and tested in vivo for their analgesic and anti-inflammatory activities. All the new compounds possess good antalgic action in the acetic acid writhing test and some terms of the series showed also fair anti-inflammatory activity in the carrageenan rat paw edema test. Ulcerogenic and irritative action on the gastrointestinal mucose, in comparison with indomethacin is low. [Copyright &y& Elsevier]

A series of 2-aryl-3-phenylamino-4,5-dihydro-2H-benz[g]indazoles was synthesized and tested for antiarrhythmic, local anaesthetic and analgesic activity. The title compounds showed a good antinociceptive activity. [Copyright &y& Elsevier]

Three series of N-acyl and N-cyclohexyl- or N-methyl or N-phenyl-thioureas of 4-substituted (methyl, phenyl, 2-pyridyl)piperazines (4–12) were synthesised according to a highly convergent one-pot procedure and tested in vivo (local anaesthetic, anti-hyperlipoproteinemic, analgesic, anti-inflammatory, antiarrythmic activities) and in vitro (antiaggregating and, for some selected derivatives, antiproliferative activities) experiments. All the test compounds showed local anaesthesia in particular 4Ar4, 5Ar4, 12Ar3 (after 5 min) and 5Ar2, 5Ar3, 9Ar4 (after 30 min) were equipotent to lidocaine. In lowering triglyceride levels, compounds 6Ar4 and 7Ar3 were more active than nicotinic acid, whereas 7Ar4 and 11Ar4 were approximately equipotent. As concerns analgesic activity, 5Ar2 and 5Ar4 were as active as indomethacin. Appreciable anti-inflammatory activity was found in 8Ar1, 5Ar2 and 11Ar2, but inferior to that of indomethacin. High levels of antiarrythmic activity, comparable with that of quinidine, were found in derivatives 4Ar2 and 10Ar1. Compounds 4Ar2 and 8Ar2, assayed in antitumor in vitro screening system at National Cancer Institute (NCI), showed significant antiproliferative activity against ACHN cell line (GI50: 0.13 μM) and NCI-H226 cell line (GI50: 1.03 μM), respectively. [Copyright &y& Elsevier]